GB2121555A

GB2121555A - A soft contact lens preserving preparation

Info

Publication number: GB2121555A
Application number: GB08229508A
Authority: GB
Inventors: Masahiro Hiranuma; Akimichi Tsukamoto; Makoto Tsuchiya
Original assignee: Hoya Lens Corp
Current assignee: Hoya Lens Corp
Priority date: 1982-06-01
Filing date: 1982-10-15
Publication date: 1983-12-21
Also published as: ES516098A0; DK432982A; NO823302L; EP0095524A1; ES8308215A1; NO170563B; NZ201761A; AU532074B1; NO170563C; JPS58209714A; JPH0261015B2

Description

1

GB 2 121 555 A

1

SPECIFICATION

A soft contact lens preserving preparation

5 This invention relates to a soft contactlens preserving composition comprising boric acid, borax and sodium chloride as essential components.

Hitherto, what has been known as a soft contactlens preservative includes the physiological saline solution and solutions having further added therein such antiseptic agent and buffer substance as thimerosal, chlorohexidine, digluconate, methylparaben, propylparaben and sorbic acid, and also tablets which are used 10 for preparing a preservative solution by dissolving a prescribed quantity of sodium chloride in a prescribed quantity of purified water or distilled water. These, however, do not give consideration to the physical properties of the lacrima, to the change in the parameters of soft contactlenses under pH and osmotic pressure, and also to the property of readily adsorbing chemical substances, especially organic compounds, which constitutes a weak point as well as a feature of soft contactlenses. Therefore, these conventional 15 preserving agents have had such shortcomings that when used, they often stimulate eyes or change parameters of a soft contactlens. As for the tablets, they presented a disadvantage of inconvenience to use, for it takes a fairly long time to dissolve them in a prescribed quantity of purified water or distilled water.

As the result we have devoted ourselves to the research in due consideration of the above mentioned matters, we attained this invention, discovering a safe preserving composition for soft contact lenses, which 20 does not stimulate (irritate) eyes and not give any significant change in the parameters of a soft contact lens.

The invention makes it possible to provide a safe preserving preparation for soft contact lenses, which contains as essential components boric acid, borax (Na2B407) and sodium chloride, and which preferably has the pH and osmotic pressure substantially equal to those of lacrima (tears), and also does not affect the lens parameters, when dissolved in a prescribed quantity of purified water or distilled water. 25 The content in purified water or distilled water of boric acid and borax (Na2B407) used in this invention after both have been dissolved is in total from about 0.3 w/v% to about 1.0 w/v%, preferably from 0.5 w/v% to 0.6 w/v%. If the total quantity of boric acid and borax exceeds 1.0 w/v%, sometimes it stimulates eyes. If the quantity is less than 0.3 w/v%, the lens parameters apt to change. Besides, if the quantity exceeds 0.5 w/v%, a bacteriostatic action by boric acid and borax will occurto give a desirable advantage as a preservative 30 solution for soft contact lenses. And if the above content of boric acid and borax is less than 1.0 w/v%, it does not cause any toxicity at all, when dropped in eyes.

The content in purified water or distilled water of sodium chloride used in this invention after it has been dissolved is from about 0.4 w/v% to about 0.8 w/v%, preferably from 0.55 w/v% to about 0.65 w/v%.

The content in purified water or distilled water of disodium salt of ethylenediamine tetraacetic acid (EDTA), 35 preferably used in this invention, is from 0.05 w/v%to 0.15 w/v%, preferably from 0.08 w/v%to 0.12 w/v%. This addition of disodium salt of EDTA to the soft contact lens preserving composition of this invention gives advantages to make the preservative solution more effective by masking the metallic ions contained in the lacrima, which ions may given an injurious effect on soft contact lenses, and in addition by promoting the bacteriostatic action of the boric acid.

40 The preserving agent is preferably granular and is preferably such that when it has been dissolved in purified water or distilled water, the pH is from 8.0 to 7.0, preferably from 7.4 to 7.2, and the osmotic pressure is from 315 to 275 mOsm. Advantageously, the pH and osmotic pressure are about 7.3 and 295 mOsm respectively, which are substantially equal to those of the lacrima. The granular agent is used by dissolving it in a prescribed quantity of purified water or distilled water.

45 The preserving composition of this invention may include appropriate binders for formulation of the granules and also suitable sterilizers such for example, as thimerosal and parabens.

The invention will now be described more in detail by way of example.

Example 1

50 1.3 g in the total weight of a granular preservative agent was prepared by formulating boric acid 39 wt.%, borax 7 wt.%, disodium salt of ethylenediamine tetraacetic acid 8 wt.%, and sodium chloride 46 wt.%, in the ratio thereof. The granular agent was dissolved in 100 ml of purified water, at which its pH was 7.3 and its osmotic pressure was 295 mOsm.

In to the preservative solution thus prepared a new soft contactlens was dipped, and change of lens 55 paramaters was measured every day when the preservative solution was renewed. At the same time,

parameter change of the other one of the same type soft contactlens dipped in a physiological saline solution was measured for composition. The results are graphically illustrated in Figure 1. In the graph, the ordinate represents diameter in mm of soft contactlens and the abscissa represents days of dipping soft contactlens. The test result in case of dipping in the preservative solution of Example 1 is indicated by line A and that in 00 case of dipping physiological saline solution is shown by line B.

Example 2

The preservative solution obtained in Example 1 and a .physiological saline solution as control were respectively dropped into the respective right and left eyes of a rabbit with three drops at one time every day 65 for one month, and occurence of eye stimulus was observed. In the result no eye stimulus such as

5

10

15

20

25

30

35

40

45

50

55

60

65

2

GB2 121 555 A

2

inflammation in the rabbit eyes was found in both cases of the preservative solution and the physiological saline solution.

Example 3

5 Regarding the preservative solution obtained in Example 1 the number of general living bacteria was 5

measured. As the result, the number of living bacteria in the preservative solution was 5- 10/ml, immediately afterthe dissolution of the granular preservative agent, but on the second day afterthe dissolution the said number decreased to 0 - 2/ml.

10 Example 4 10

The granular preservative agent made up according to the content ratio of Example 1 into the total weight of 1.3 g and a tablet prepared by the same manner into the total weight of 1.3 g were tested on their solubilities when they were dissolved in 100 ml of purified water. The result is shown in Table 1.

15 TABLE 1 15

Time required for dissolution

Not stired Stirred

20 20

Granule 5-10min 1-2min

Tablet Morethan 10 min 4-5 min

25 The chemical means of certain of the substances referred to in the specification are as follows: 25

thimerosal - ethyl(2-mercaptobenzoate-s)mercury sodium salt or ((o-carboxypheny!)thio)ethyl mercury sodium salt chlorohexidine - N, N"- bis (4-chlorophenyl)-3,12-diimino-2,4,11,13-tetraazatetradecane-diimidamide,

30 or 30

1,1'-hexamethylenebis(5-(p-chlorophenyl)biguanide)

methylparaben - 4-hydroxybenzoic acid methyl ester propylparaben - 4-hydroxybenzoic acid propyl ester

35 The unit of osmotic pressure used in the specification is the mOsm., where 1 mOsm = 10~3 Osm. 1 Osm 35 (more exactly 1 Osm/kg) is the osmotic pressure when 1 mole of non-electrolyte solute is dissolved in 1 kg of water.

The ratio of boric acid : borax in the preparation of the invention may vary depending on the desired pH and on the other ingredients present. Preferably this ratio is from 5 :1 to 6 :1 by weight.

40 The preparation according to the invention is preferably granular and advantageously comprises the 40

following four constituents, the percentage by weight of each constituent being in the following ranges.

Boric Acid 54.5-18.3, preferably 39.4-34.1 Borax 12.2- 3.7, preferably 7.9- 6.5 NaCI 24.2 - 73.4, preferably 43.3 - 52.8

45 EDTA-2Na 9.1 - 4.6, preferably 9.4 - 6.5 45

Such a preparation may be dissolved in an appropriate amount of pure water to make a final solution having proportions of constituents in accordance with the present invention.

The present invention also provides a preserving solution made by dissolving in water that is sufficiently pure to have no adverse effects on the human eye a composition according to the invention. The invention

50 further provides a preserving solution for soft contact lenses comprising a solution in water of about 0.4 to 50 about 0.8 w/v% of sodium chloride and from about 0.3 to about 1.0 w/v% in total of boric acid and borax (NA2B407I0H20).

The invention also provides a preserving solution according to the invention having at least one soft contact lens therein.

55 55

Claims

1. A soft contactlens preserving composition comprising sodium chloride, boric acid and borax, which is so formulated as to be in the proportion of from about 0.4 to about 0.8 w/v% of NaCI and from about 0.3 to

00 about 1.0 w/v% in total of boric acid and borax, when the composition is dissolved in a prescribed amount of 60 pure water.

2. The composition according to Claim 1, wherein said proportion is preferably from 0.55 to 0.65 w/v% of NaCI and preferably from 0.5 to 0.6 w/v% in total of boric acid and borax.

3. The soft contactlens preserving composition according to Claims 1 or 2, which further contains

05 disodium salt of ethylenediamine tetraacetic acid. 65

GB 2 121 555 A

4. The soft contactlens preserving composition according to Claims 1,2 or 3, which is in the granular form.

5. A soft contactlens preserving composition according to Claim 4, whose pH and osmotic pressure are so controlled as to be substantially equal to those of the lacrima when said composition in the granular form

5 is dissolved in a prescribed quantity of purified water or distilled water. 5

6. A soft contactlens preserving composition according to Claims 4 to 5, characterized in that, when a contactlens is preserved in the preservative solution having dissolved therein said granular composition in a prescribed quantity of purified water or distilled water, parameters of said contactlens substantially does not change.

10

7. A soft contact lens preserving composition as claimed in claim 3 wherein the percentage by weight of iq each constituent is within the following ranges:

boric acid 54.5-18.3 borax 12.2- 3.7 NaCI 24.2-73.4

15 EDTA/2Na 9.1 - 4.6 15

8. A soft contact lens preserving composition as claimed in claim 7 wherein the ranges of percentages are:

boric acid 39.4-34.1 borax 7.9- 6.5

20 NaCI 43.4-52.8 20

EDTA/2Na 9.4 - 6.5

9. A soft contact lens preserving composition wherein the weight ratio of boric acid to borax is 5 :1 to 6 :

I.

10. A soft contact lens preserving composition as claimed in claim 1 and substantially as described

25 herein. 25

11. A soft contact lens preserving composition substantially as described in Example 1.

12. A preserving solution made by dissolving in water a composition as claimed in any one of claims 1 to

II.

13. A preserving solution for soft contact lenses comprising a solution in water of about 0.4 to about 0.8

30 w/v% of sodium chloride and from about 0.3 to about 1.0 w/v% in total of boric acid and borax 30

(Na2B407-l0H20).

14. A solution as claimed in claim 13, wherein the proportions are from 0.55 to 0.65 w/v% of sodium chloride and from 0.5 to 0.6 w/v% in total of boric acid and borax.

15. A solution as claimed in claim 13 or claim 14 which also contains the disodium salt of

35 ethylenediamine tetraacetic acid. 35

16. A solution as claimed in any one of claims 12 to 16, which has a pH of from 8.0 to 7.0.

17. A solution as claimed in claim 16, wherein the pH is from 7.4 to 7.2.

18. A solution as claimed in any one of claims 12 to 17, having an osmotic pressure of from 315 to 275 mOsm.

40

19. A solution as claimed in claim 13 and substantially as described herein. 40

20. A solution as claimed in claim 13 and substantially as described in Example 1.

21. A solution as claimed in any one of claims 12 to 20 having at least one soft contact lens therein.

Printed for Her Majesty's Stationery Office, by Croydon Printing Company Limited, Croydon, Surrey, 1983. Published by The Patent Office, 25 Southampton Buildings, London, WC2A 1AY, from which copies may be obtained.